School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.
Molecules. 2020 Mar 15;25(6):1334. doi: 10.3390/molecules25061334.
An aqueous polyvinyl alcohol (PVA)/chitosan (CHT)/polyhexamethylene biguanide (PHMB) blends (PVA/CHT/PHMB blends) has been developed as a potential low dose topical antibacterial formulation with enhanced antimicrobial effect. The preparation of PVA/CHT/PHMB blends was quite facilely, with just dissolved PVA, CHT, PHMB in water in order. There was the aggregates with 100 nm size around induced by phase separation in the blends and an aqueous two-phase system (ATPS) formed, as non-ionic polymer PVA formed a continuous phase and cationic polymer CHT and PHMB formed dispersed phases. The minimum inhibitory concentration (MIC) of PHMB in the PVA/CHT/PHMB blends was 0.5μg/mL, which was four times lower than the MIC of PHMB individually. A phase separation increased zeta potential mechanism was proposed to explain the enhanced antibacterial activities. In addition, the blends could easily form film on the skin surface with good water vapor permeability and be used as a liquid bandage to accelerate the scratch wound healing process of nude mouse. These findings provide experimental evidence that the PHMB-functionalized blends could be further explored as low-dose topical antibacterial formulations, and the nano-sized phase separation strategy could be used to design novel low-dose topical antibacterial formulations with an enhanced antimicrobial effect.
一种水性聚乙烯醇(PVA)/壳聚糖(CHT)/聚六亚甲基双胍(PHMB)共混物(PVA/CHT/PHMB 共混物)已被开发为具有增强抗菌效果的潜在低剂量局部抗菌制剂。PVA/CHT/PHMB 共混物的制备非常简单,只需将 PVA、CHT、PHMB 溶解在水中即可。共混物中会发生相分离,形成 100nm 左右的聚集体,并形成双水相体系(ATPS),其中非离子聚合物 PVA 形成连续相,阳离子聚合物 CHT 和 PHMB 形成分散相。PVA/CHT/PHMB 共混物中 PHMB 的最小抑菌浓度(MIC)为 0.5μg/mL,比单独使用 PHMB 时低 4 倍。提出了相分离增加zeta 电位的机制来解释增强的抗菌活性。此外,共混物可在皮肤表面轻松形成薄膜,具有良好的水蒸气透过性,并可用作液体绷带,以加速裸鼠划痕伤口的愈合过程。这些发现为 PHMB 功能化共混物可进一步探索作为低剂量局部抗菌制剂提供了实验依据,纳米级相分离策略可用于设计具有增强抗菌效果的新型低剂量局部抗菌制剂。